|本期目录/Table of Contents|

[1]韩 谢,邵开元,胡文祥*.小檗碱结构修饰的研究进展[J].武汉工程大学学报,2018,40(01):1-7.[doi:10. 3969/j. issn. 16742869. 2018. 01. 001]
 HAN Xie,SHAO Kaiyuan,HU Wenxiang*.Advances in Structural Modification of Berberine[J].Journal of Wuhan Institute of Technology,2018,40(01):1-7.[doi:10. 3969/j. issn. 16742869. 2018. 01. 001]
点击复制

小檗碱结构修饰的研究进展(/HTML)
分享到:

《武汉工程大学学报》[ISSN:1674-2869/CN:42-1779/TQ]

卷:
40
期数:
2018年01期
页码:
1-7
栏目:
化学与化学工程
出版日期:
2018-02-25

文章信息/Info

Title:
Advances in Structural Modification of Berberine
文章编号:
20180101
作者:
韩 谢12邵开元2胡文祥*123
1. 武汉工程大学化工与制药学院,湖北 武汉 430205;2. 北京神剑天军医学科学院京东祥鹄微波化学联合实验室,北京 101601;3. 中国人民解放军战略支援部队航天系统部,北京 100101
Author(s):
HAN Xie12 SHAO Kaiyuan2 HU Wenxiang*123
1. School of Chemical Engineering and Pharmacy, Wuhan Institute of Technology, Wuhan 430205, China; 2. Jingdong Xianghu Microwave Chemistry Union Laboratory, Beijing Excalibur Space Military Academy of Medical Sciences, Beijing 101601, China;3. Space Systems Division, Strategic Support Troops, Chinese People’s Liberation Army, Beijing 100101, China
关键词:
小檗碱 结构修饰 药理作用
Keywords:
berberine structural modification pharmacological effects
分类号:
O625.6
DOI:
10. 3969/j. issn. 16742869. 2018. 01. 001
文献标志码:
A
摘要:
小檗碱作为一种生物碱具有重要的医用价值,已广泛的应用于消炎、降血脂、降血糖、抗癌等诸多方面,而大量药理研究进一步表明:对其结构进行修饰改造可以提高其生物活性,使其具有更加优秀的药用功效,更加易于临床使用。同时,大量小檗碱衍生物的合成可望进一步深入了解小檗碱作用于人体的生物机制,以便进一步扩展其应用范围。介绍了近年小檗碱结构修饰研究进展,重点介绍在其分子结构中N(7)、C(8)、C(9)、C(12)和C(13)位点的结构修饰方法。此外,还介绍了修饰后生物活性的变化,以及一些具有较好生物活性的小檗碱衍生物,旨在为进一步深入开展以药效机制为基础的小檗碱结构改造和创新药物研究提供重要的参考信息。
Abstract:
Berberine as an alkaloid has been widely applied in fields of anti-inflammatory anti-hyperlipidemia, anti-hypoglycemia and anti-cancer. A large number of pharmacological studies demonstrated that the structural modification of berberine could improve its biological activity with excellent medicinal efficacy in clinical applications. Meanwhile, the numerous syntheses of berberine derivatives are expected to help people further understand the biological mechanism of berberine on the human body, and extend the application ranges of berberine. By reviewing the research progress of structural modification of berberine, this paper focuses on the structural modification method for N(7), C(8), C(9), C(12) and C(13) sites in the molecular structures. Besides, the modified biological activity and the berberine derivatives with better bioactivity are introduced, providing systematic information for further studies on structural modification of berberine for developing new drug based on its pharmacodynamic mechanisms.

参考文献/References:

[1] 郑洪艳, 徐为人. 小檗碱药理作用研究进展[J]. 中草药, 2004, 35(6):708-711. [2] 李波, 朱维良, 陈凯先. 小檗碱及其衍生物的研究进展[J]. 药学学报, 2008, 43(8):773-787. [3] AMIN A H, SUBBAIAH T V, ABBASI K M. Berberine sulfate: antimicrobial activity, bioassay, and mode of action[J]. Canadian Journal of Microbiology, 1969, 15(9):1067-1076. [4] 张灿, 黄文龙. 原小檗碱季铵类化合物的合成及抗心律失常活性研究[J]. 中国药科大学学报, 2003, 34(1):7-12. [5] LIN C C, NG L T, HSU F F, et al. Cytotoxic effects of Coptis chinensis and Epimedium sagittatum extracts and their major constituents (berberine, coptisine and icariin) on hepatoma and leukaemia cell growth[J]. Clinical & Experimental Pharmacology & Physiology, 2004, 31(1/2):65-69. [6] YIN J, HU R, CHEN M, et al. Effects of berberine on glucose metabolism in vitro. [J]. Metabolism: Clinical and Experimental, 2002, 51(11):1439-1443. [7] KONG W, WEI J, ABIDI P, et al. Berberine is a novel cholesterol-lowering drug working through a unique mechanism distinct from statins [J]. Nature Medicine, 2004, 10(12):1344-1451. [8] 胡文祥,徐楠楠,王卓,等. 一种降糖及降脂药物组合物及其制备方法:中国,200710179390.3[P]. 2007-12-12. [9] 张磊, 王京, 聂晶, 等. 四氢小檗碱衍生物的合成与表征[J]. 广东化工, 2014, 41(15):36-37. [10] 王冬梅, 魏金钊, 范宝妍,等. 四氢黄连碱型季铵化合物的合成及生物活性研究[J]. 药学学报, 2012(12):1640-1645. [11] 杨勇. 8-烷基小檗碱同系物的合成与药理活性[D]. 重庆:西南大学, 2008. [12] 胡宇莉. 8-十六烷基小檗碱的合成和药代动力学研究[D]. 重庆:西南大学, 2015. [13] IWASSA K, KAMIGAUCHI M. 13-hydroxylation of tetrahydroberberine in cell suspension cultures of some Corydalis, species[J]. Phytochemistry, 1996, 41(6):1511-1515. [14] 韩谢, 邵开元, 胡文祥. 微波辐射合成9-氧-2-溴乙基小檗碱工艺研究[J]. 微波化学, 2017,1(1): 8-14. [15] CHEN Z, YE X, YI J, et al. Synthesis of 9-O-glycosyl-berberine derivatives and bioavailability evaluation[J]. Medicinal Chemistry Research, 2012, 21(8):1641-1646. [16] KIM S H, LEE S J, LEE J H, et al. Antimicrobial activity of 9-O-acyl- and 9-O-alkylberberrubine derivatives. [J]. Planta Medica, 2002, 68(3):277-281. [17] ZHANG S, WANG X, YIN W, et al. Synthesis and hypoglycemic activity of 9-O-(lipophilic group substituted) berberine derivatives[J]. Bioorganic & Medicinal Chemistry Letters, 2016, 26(19):4799-4803. [18] MISTRY B, KEUM Y S, KIM D H. Synthesis and biological evaluation of berberine derivatives bearing 4-aryl-1-piperazine moieties[J]. Journal of Chemical Research, 2015, 39(8):470-474. [19] SHI A, HUANG L, LU C, et al. Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and β-amyloid aggregation inhibitors[J]. Bioorganic & Medicinal Chemistry, 2011, 19(7):2298-2305. [20] HUANG M Y, LIN J, HUANG Z J, et al. Design, synthesis and anti-inflammatory effects of novel 9-O-substituted-berberine derivatives[J]. Medlicinal Chemistry Communicaiton, 2016, 7(4):730-731. [21] HUANG L, LUO Z, HE F, et al. Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase[J]. Bioorganic & Medicinal Chemistry Letters, 2010, 20(22):6649-6652. [22] FRERICHS G. Beitr?ge zur kenntnis des berberins. ueber berberrubin[J]. Archiv Der Pharmazie, 2010, 251(5):321-339. [23] ZHOU X, CHEN M, ZHENG Z, et al. Synthesis and evaluation of novel 12-aryl berberine analogues with hypoxia-inducible factor-1 inhibitory activity[J]. RSC Advances, 2017, 43(7):26921-26929. [24] 丁阳平, 叶小利, 周洁, 等. 小檗碱衍生物合成及生理活性研究进展[J]. 有机化学, 2012, 32(4):677-685. [25] PARK K D, CHO S J, MOON J S, et al. Synthesis and antifungal activity of a novel series of 13-(4-isopropylbenzyl)berberine derivatives[J]. Bioorganic & Medicinal Chemistry Letters, 2010, 20(22):6551-6554. [26] DING Y, YE X, ZHU J, et al. Structural modification of berberine alkaloid and their hypoglycemic activity[J]. Journal of Functional Foods, 2014, 7(1):229-237. [27] BUROV O N,KURBATOV S V,KLETSKII M E, et al. Synthesis and structure of dihydroberberine nitroaryl derivatives-potential ligands for G-quadruplexes[J]. Chemistry of Heterocyclic Compounds, 2017,53(3):335-340. [28] 赵午莉, 李阳彪, 李迎红,等. 13-取代小檗碱衍生物的合成及其抗肿瘤活性研究[J]. 中国医药导报, 2013, 10(18):17-20.

相似文献/References:

备注/Memo

备注/Memo:
作者简介:韩 谢,硕士研究生。E-mail:642697718@qq.com*通讯作者:胡文祥,博士,教授。E-mail:huwx66@163.com引文格式:韩谢,邵开元,胡文祥. 小檗碱结构修饰的研究进展[J]. 武汉工程大学学报,2018,40(1):1-7.
更新日期/Last Update: 2018-02-01